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1. (WO2012172473) CYSTEINE PROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2012/172473 International Application No.: PCT/IB2012/052939
Publication Date: 20.12.2012 International Filing Date: 11.06.2012
IPC:
C07D 231/40 (2006.01) ,A61K 31/415 (2006.01) ,A61K 31/4155 (2006.01) ,A61K 31/4164 (2006.01) ,A61P 3/06 (2006.01) ,A61P 7/00 (2006.01) ,A61P 11/06 (2006.01) ,A61P 37/08 (2006.01) ,C07D 233/88 (2006.01) ,C07D 305/08 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
40
Acylated on said nitrogen atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
4155
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3
Drugs for disorders of the metabolism
06
Antihyperlipidemics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11
Drugs for disorders of the respiratory system
06
Antiasthmatics
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
08
Antiallergic agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
66
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
88
Nitrogen atoms, e.g. allantoin
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
305
Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
02
not condensed with other rings
04
having no double bonds between ring members or between ring members and non-ring members
08
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring atoms
Applicants:
MEDIVIR UK LTD; Chesterford Research Park Chesterford Essex CB10 1XL, GB (AllExceptUS)
GRABOWSKA, Urszula [GB/GB]; GB (UsOnly)
HEWITT, Ellen [GB/GB]; GB (UsOnly)
JÖNSSON, Daniel [SE/SE]; SE (UsOnly)
KLASSON, Björn [SE/SE]; SE (UsOnly)
WIKTELIUS, Daniel [SE/SE]; SE (UsOnly)
Inventors:
GRABOWSKA, Urszula; GB
HEWITT, Ellen; GB
JÖNSSON, Daniel; SE
KLASSON, Björn; SE
WIKTELIUS, Daniel; SE
Priority Data:
115053413.06.2011SE
Title (EN) CYSTEINE PROTEASE INHIBITORS
(FR) INHIBITEURS DE LA CYSTÉINE PROTÉASE
Abstract:
(EN) Compounds of the formula (I) wherein One of A1 and A2 is N-CH3 and the other is CH; R1 is C1-C6alkyl, C1-C6haloalkyl, C3-C6cycloalkyl or oxetan-3-yl, wherein C3-C6cycloalkyl is optionally substituted with one, two or three fluoro or with CF3; R2a and R2b are independently selected from H, halo, C1-C4alkyl, C1-C4haloalkyl and C1- C4alkoxy; R3 is CH3 or F; n is 1, 2, 3 or 4; or a pharmaceutically acceptable salt, hydrate or N-oxide thereof for the use in the prophylaxis and/or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.
(FR) La présente invention concerne des composés de formule (I) dans laquelle: un parmi A1 et A2 est N-CH3 et l'autre est CH; R1 est alkyle C1-C6, haloalkyle C1-C6, cycloalkyle C3-C6 ou oxétan-3-yle, le cycloalkyle C3-C6 étant éventuellement substitué avec un, deux ou trois groupes fluoro ou avec CF3; R2a et R2b sont indépendamment choisis parmi H, halo, alkyle C1-C4, haloalkyle C1-C4 et alcoxy C1-C4; R3 est CH3 ou F; n est 1, 2, 3 ou 4; ou un sel, hydrate ou N-oxyde pharmaceutiquement acceptable de ceux-ci pour une utilisation dans la prophylaxie et/ou le traitement d'un trouble caractérisé par une expression ou activation inappropriée de la cathepsine S.
front page image
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)